MX2017009028A - Formas cristalinas novedosas de maleato de neratinib y procedimiento de preparacion de las mismas. - Google Patents
Formas cristalinas novedosas de maleato de neratinib y procedimiento de preparacion de las mismas.Info
- Publication number
- MX2017009028A MX2017009028A MX2017009028A MX2017009028A MX2017009028A MX 2017009028 A MX2017009028 A MX 2017009028A MX 2017009028 A MX2017009028 A MX 2017009028A MX 2017009028 A MX2017009028 A MX 2017009028A MX 2017009028 A MX2017009028 A MX 2017009028A
- Authority
- MX
- Mexico
- Prior art keywords
- preparation
- crystal form
- new crystal
- method therefor
- maleate
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 3
- 238000002360 preparation method Methods 0.000 title abstract 3
- VXZCUHNJXSIJIM-MEBGWEOYSA-N (z)-but-2-enedioic acid;(e)-n-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound OC(=O)\C=C/C(O)=O.C=12C=C(NC(=O)\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 VXZCUHNJXSIJIM-MEBGWEOYSA-N 0.000 title abstract 2
- 229950008835 neratinib Drugs 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 abstract 1
- 238000005457 optimization Methods 0.000 abstract 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/41—Preparation of salts of carboxylic acids
- C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/42—Separation; Purification; Stabilisation; Use of additives
- C07C51/43—Separation; Purification; Stabilisation; Use of additives by change of the physical state, e.g. crystallisation
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/145—Maleic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La presente invención se refiere a formas cristalinas novedosas de maleato de Neratinib y el método de preparación de las mismas; las formas cristalinas novedosas de maleato del compuesto de la Fórmula (I) en la presente invención tienen alta solubilidad, buena estabilidad, buena procesabilidad, fácil procedimiento post-tratamiento y otras propiedades favorables; el método de preparación es simple, de bajo costo, y tiene un valor importante para la optimización y desarrollo futuros del fármaco. (ver Fórmula).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510012580.0A CN105367552A (zh) | 2015-01-09 | 2015-01-09 | 来那替尼马来酸盐的新晶型及其制备方法 |
| PCT/CN2016/070472 WO2016110270A1 (zh) | 2015-01-09 | 2016-01-08 | 来那替尼马来酸盐的新晶型及其制备方法 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2017009028A true MX2017009028A (es) | 2017-09-27 |
Family
ID=55370239
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017009028A MX2017009028A (es) | 2015-01-09 | 2016-01-08 | Formas cristalinas novedosas de maleato de neratinib y procedimiento de preparacion de las mismas. |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10246437B2 (es) |
| EP (1) | EP3243819A4 (es) |
| JP (1) | JP2018501289A (es) |
| CN (2) | CN105367552A (es) |
| CA (1) | CA2973853C (es) |
| IL (1) | IL253360A0 (es) |
| MX (1) | MX2017009028A (es) |
| WO (1) | WO2016110270A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018005418A1 (en) | 2016-06-27 | 2018-01-04 | Pliva Hrvatska D.O.O. | Solid state forms of neratinib and salts thereof |
| CN108299391A (zh) * | 2016-08-25 | 2018-07-20 | 杭州领业医药科技有限公司 | 来那替尼二马来酸盐的晶型及其制备方法和药物组合物 |
| WO2018134843A1 (en) * | 2017-01-23 | 2018-07-26 | Msn Laboratories Private Limited, R&D Center | Polymorphic forms of (e)-n-{4-[3-chloro-4-((pyridin-2-yl methoxy)anilino]-3-cyano-7- ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide, its maleate salt and process for preparation thereof |
| WO2018189695A1 (en) * | 2017-04-11 | 2018-10-18 | Lupin Limited | Neratinib crystalline forms and process for preparation thereof |
| WO2019015394A1 (zh) * | 2017-07-17 | 2019-01-24 | 苏州科睿思制药有限公司 | 一种来那替尼单马来酸盐的晶型及其制备方法和用途 |
| US11034656B2 (en) | 2017-11-20 | 2021-06-15 | Teligene Ltd. | Maleate salts of (E)-N-(3-cyano-7-ethoxy-4-((4-phenoxyphenyl)amino) quinolin-6-yl)-4-(dimethylamino)but-2-enamide and crystalline forms thereof |
| CN107698563B (zh) * | 2017-11-23 | 2020-10-30 | 江苏创诺制药有限公司 | 制备马来酸来那替尼晶型的方法 |
| CN108299394A (zh) * | 2018-02-28 | 2018-07-20 | 江苏创诺制药有限公司 | 来那替尼二马来酸盐晶型及其制备方法 |
| CN110357855A (zh) * | 2018-03-26 | 2019-10-22 | 江苏创诺制药有限公司 | 一种来那替尼盐酸盐晶型及其制备方法 |
| CN109053683A (zh) * | 2018-07-27 | 2018-12-21 | 苏州晶云药物科技股份有限公司 | 来那替尼马来酸盐晶型c的制备方法以及来那替尼马来酸盐晶型c |
| KR20210081367A (ko) * | 2018-10-22 | 2021-07-01 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 티로신 키나아제 억제제의 말레에이트의 결정 형태 및 이의 제조 방법 |
| CN111087384A (zh) * | 2018-10-23 | 2020-05-01 | 浙江京新药业股份有限公司 | 一种环己烷衍生物马来酸盐的晶型 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2609186A1 (en) * | 2005-05-25 | 2006-11-30 | Wyeth | Methods of synthesizing substituted 3-cyanoquinolines and intermediates thereof |
| WO2006127205A2 (en) * | 2005-05-25 | 2006-11-30 | Wyeth | Methods of preparing 3-cyano-quinolines and intermediates made thereby |
| US8022216B2 (en) * | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
-
2015
- 2015-01-09 CN CN201510012580.0A patent/CN105367552A/zh active Pending
-
2016
- 2016-01-08 JP JP2017536527A patent/JP2018501289A/ja active Pending
- 2016-01-08 US US15/542,597 patent/US10246437B2/en not_active Expired - Fee Related
- 2016-01-08 MX MX2017009028A patent/MX2017009028A/es unknown
- 2016-01-08 CN CN201680014229.8A patent/CN107428727B/zh active Active
- 2016-01-08 CA CA2973853A patent/CA2973853C/en not_active Expired - Fee Related
- 2016-01-08 EP EP16734930.7A patent/EP3243819A4/en not_active Withdrawn
- 2016-01-08 WO PCT/CN2016/070472 patent/WO2016110270A1/zh not_active Ceased
-
2017
- 2017-07-09 IL IL253360A patent/IL253360A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2973853C (en) | 2019-08-27 |
| EP3243819A1 (en) | 2017-11-15 |
| EP3243819A4 (en) | 2018-06-27 |
| CN105367552A (zh) | 2016-03-02 |
| JP2018501289A (ja) | 2018-01-18 |
| US20180265495A1 (en) | 2018-09-20 |
| CN107428727B (zh) | 2021-04-27 |
| IL253360A0 (en) | 2017-09-28 |
| US10246437B2 (en) | 2019-04-02 |
| CA2973853A1 (en) | 2016-07-14 |
| CN107428727A (zh) | 2017-12-01 |
| WO2016110270A1 (zh) | 2016-07-14 |
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